Guide to Opioid Replacement Therapy

man talking with doctor

The Centers for Disease Control and Prevention, or CDC, has labeled prescription drug abuse an epidemic in the United States, with over 2 million Americans addicted to pain pills, and 44 people dying every day from a prescription opioid overdose.

Tighter regulations of narcotic painkillers and the introduction of abuse-deterrent medications in recent years have made popular drugs of abuse, such as OxyContin, more difficult and expensive to obtain and crush to snort, smoke, or inject.

Heroin, a dangerous opioid street drug especially common during the 1960s, seems to be making a comeback as the number of heroin abusers jumped from 373,000 to 669,000 from 2007 to 2012, TIME magazine reports. The number of heroin overdose deaths has also spiked 45 percent between 2006 and 2010. Aside from the potential for a fatal overdose, heroin has many short-term and long-term side effects and negative consequences surrounding its abuse. For instance, the World Health Organization (WHO), reports that worldwide around 10 percent of new HIV infections may be caused by injecting a drug such as heroin.

Heroin and other street drugs are also obtained by illegal or criminal means, as the Bureau of Justice Statistics (BJS) reported that in 2004, approximately 17 percent of state prisoners and 18 percent of federal prisoners committed their most recent offense while trying to obtain money for drugs.

Injecting drugs is the most dangerous methods of abuse with the most potential side effects, such as overdose, spread of infectious disease, and engaging in criminal activities to obtain and use them. Violent behaviors and crime are often tied to IV drug users. The National Institute on Drug Abuse (NIDA) estimates that drug abuse costs American society $181 billion each year in lost workplace production, criminal justice costs, and health care costs. Injection drug users generally have difficulties retaining jobs, fulfilling family obligations, and have legal difficulties and health problems.

Opioid replacement therapy is a treatment option that seeks to replace dangerous drugs like heroin with legal and less euphoric, longer-acting opioids, thus decreasing possible criminal behavior and the potential health risks associated with illicit drug abuse.

Opioids and the brain

man talking with support groupShort-acting opioids, such as heroin, Vicodin, Percocet, and OxyContin, have relatively short half-lives, meaning that they take effect rather quickly and also leave the bloodstream within a few hours. Regular use of opioids can create a tolerance to them, and users will need to take higher doses each time in order to produce the desired effects. This can also lead to a dependence on opioids as the brain’s motivation and reward centers and pathways are altered.

Opioid drugs work by acting on opioid receptors in the brain that are partially responsible for emotional regulation and pain sensations. When the production of natural neurotransmitters, or the brain’s chemical messengers, is disrupted with repeated opioid drug use over time, changes will occur in the brain’s chemical pathways, as the brain will now rely on the drugs instead of naturally occurring cells.

When opioids are removed, drug cravings and uncomfortable withdrawal symptoms will start as the brain struggles to regain balance without drugs. These withdrawal symptoms are both physical and psychological, and they will differ in intensity and duration depending on the type of drug taken, length of time abused, amount taken, method of abuse, and personal physiological factors. Opioid withdrawal symptoms often include:

    • Nausea and/or vomiting
    • Diarrhea
    • Abdominal cramps
    • Muscle aches
    • Sweating and chills
    • Runny nose
    • Yawning
    • Dilated pupils
    • Irregular heart rate
    • Restlessness
    • Anxiety
    • Depression
    • Irritability
    • Trouble sleeping
    • Drug cravings

  • In order to avoid these negative side effects, opioid abuse should never be stopped suddenly. Instead, opioids with longer half-lives can be introduced to engage opioid receptors without the “high” in order to slowly detox and regain healthy brain function. For optimal results, detox, or the removal of opioid drugs from the system, should be monitored by a medical professional and performed through a specialized detox facility. The longer you have been using opioids, and the more dependent your brain and body are to the drugs, may determine the level of detox treatment that will best suit you

Detox programs may be either inpatient, where you stay on site and receive 24-hour medical supervision, or outpatient, where you go home to sleep at night. The use of medications, such as other opioids, during detox is called medically assisted detox and should be closely monitored and continually reevaluated to ensure safety and effectiveness. Opioid replacement therapy usually utilizes either methadone or buprenorphine during detox and maintenance treatment programs. These are longer-acting opioids that stay in the system for prolonged periods of time.


Methadone is a full opioid agonist with a long half-life, generally remaining effective for 24-36 hours. It has been used for many years for opioid replacement therapy, as it does not have the same intoxicating effect as other shorter-acting opioids. Methadone can be dispensed in tablet form once per day from federally regulated clinics. Being an opioid agonist, methadone still binds to opioid receptors in the brain, activating them and therefore largely eliminating withdrawal symptoms and drug cravings.

Numerous studies have indicated that methadone maintenance therapy, or MMT as it is often called, is an effective treatment for heroin dependence, increasing retention in substance abuse programs and reducing heroin abuse, as published in the Cochran Database of Systematic Reviews.

Length of time spent in treatment has long been understood to be related to relapse and recovery rates. The more time you spend in a substance abuse treatment program, the more successful your recovery will likely be.

Methadone is a Schedule II controlled substance by the Drug Enforcement Administration (DEA), indicating its medicinal use but also its potential for diversion and abuse. MMT provides a legal and less dangerous alternative to heroin or injection opioid abuse, with success rates as high as 60-90 percent, the California Society of Addiction Medicine (CSAM) reports.

Long-term methadone use is not without its critics, however. Methadone is still an opioid, and it is often abused or misused with negative consequences. Methadone use should be closely supervised and monitored. It also should be combined with psychotherapeutic methods in order to deter abuse and work toward abstinence and a sustained recovery from addiction.


Bottle of Pills on whiteIn 2002, the U.S. Food and Drug Administration, or FDA, approved the use of Subutex and Suboxone through the Drug Abuse Treatment Act (DATA) of 2000. These opioid dependency treatment medications can be prescribed by your doctor and obtained through a pharmacy as an alternative to methadone, which is available via methadone clinics, thereby increasing access to opioid replacement therapy.

Buprenorphine is a partial opioid agonist that acts on opioid receptors in the brain to a lesser effect than full agonists do, meaning that it is effective in reducing drug cravings and withdrawal symptoms but does not produce euphoric or intoxicating feelings. Like methadone, buprenorphine has a longer half-life and can remain in your system for 24-72 hours. It also has a ceiling effect, which means that even if you take more in an effort to get “high,” the effects will plateau at a certain level, preventing the high. Subutex and Suboxone are both sublingual film strips that are difficult to alter and abuse.

Subutex contains primarily buprenorphine, and it is often used during opioid detox. Suboxone is four parts buprenorphine and one part naloxone, which is a partial opioid antagonist, meaning that it blocks opioids from receptors in the brain and can precipitate withdrawal if injected or abused with other opioids.

Another buprenorphine/naloxone product approved by the FDA in 2013 is Zubsolv, which comes in tablet form.

The DEA classifies buprenorphine as a Schedule III controlled substance and publishes that 9.3 million buprenorphine prescriptions were dispensed in 2012. Like methadone, buprenorphine can increase retention in substance abuse treatment programs while potentially reducing relapse and helping people to lead fulfilling and productive lives.

The National Survey on Drug Use and Health (NSDUH) estimates that there were 22.7 million Americans aged 12 and older who needed treatment for a substance abuse or dependency issue; however, only 2.5 million actually received the necessary treatment at a specialized facility. Opioid replacement therapy can help you to reach a healthy and stable physical level, and it should be combined with psychotherapies and counseling sessions to address the emotional components of drug abuse and addiction.

A successful drug abuse treatment program may include both the use of pharmaceuticals and behavioral therapies to help you or your loved one retrain your brain and make healthy lifestyle choices.

The Recovery Village is a frontrunner in evidence-based treatment models. Highly trained professionals utilize traditional and alternative methods in order to achieve long-lasting results. Admission specialists are standing by to answer any questions you may have about the range of substance abuse treatment programs offered.

Guide to Opioid Replacement Therapy
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